Applications of γ, δ-unsaturated ketones synthesized by copper-catalyzed cascade addition of vinyl Grignard reagents to esters

A Douchez, A Geranurimi… - Accounts of Chemical …, 2018 - ACS Publications
Conspectus γ, δ-Unsaturated ketones, so-called homoallylic ketones, have served as
versatile building blocks for the synthesis of a variety of heterocycles, carbocycles, natural …

Allosteric modulator leads hiding in plain site: Developing peptide and peptidomimetics as GPCR allosteric modulators

KM Olson, JR Traynor, A Alt - Frontiers in Chemistry, 2021 - frontiersin.org
Allosteric modulators (AMs) of G-protein coupled receptors (GPCRs) are desirable drug
targets because they can produce fewer on-target side effects, improved selectivity, and …

Expanding Structure–Activity Relationships of Human Urotensin II Peptide Analogues: A Proposed Key Role of the N-Terminal Region for Novel Urotensin II Receptor …

F Merlino, A Secondo, E Mitidieri… - Journal of Medicinal …, 2024 - ACS Publications
While the urotensinergic system plays a role in influencing various pathologies, its potential
remains untapped because of the absence of therapeutically effective urotensin II receptor …

Functional selectivity revealed by N-methylation scanning of human urotensin II and related peptides

F Merlino, É Billard, AM Yousif, S Di Maro… - Journal of medicinal …, 2019 - ACS Publications
In accordance with their common but also divergent physiological actions, human urotensin
II (1) and urotensin II-related peptide (2) could stabilize specific urotensin II receptor (UTR) …

Discovery of new allosteric modulators of the urotensinergic system through substitution of the urotensin II-related peptide (URP) phenylalanine residue

E Billard, TE Hébert, D Chatenet - Journal of Medicinal Chemistry, 2018 - ACS Publications
Urotensin II (UII) and urotensin II-related peptide (URP) are functionally selective,
suggesting that these two hormones might play distinct physiological role through different …

Exploration of the urocontrin A scaffold yields new urotensinergic system allosteric modulator and competitive antagonists

E Billard, TE Hébert, D Chatenet - Biochemical Pharmacology, 2023 - Elsevier
The urotensinergic system, involved in the development and/or progression of numerous
pathological conditions, is composed of one G protein-coupled receptor (UT) and two …

Towards targeting the urotensinergic system: overview and challenges

H Nassour, M Iddir, D Chatenet - Trends in Pharmacological Sciences, 2019 - cell.com
The urotensinergic system, comprised of a G protein-coupled receptor (UT) and two
endogenous ligands named urotensin II (UII) and urotensin II-related peptide (URP), has …

Lipidated peptides derived from intracellular loops 2 and 3 of the urotensin II receptor act as biased allosteric ligands

H Nassour, TA Hoang, RD Martin… - Journal of Biological …, 2021 - ASBMB
Over the last decade, the urotensinergic system, composed of one G protein-coupled
receptor and two endogenous ligands, has garnered significant attention as a promising …

Insights into the Molecular Determinants Involved in Urocontrin and Urocontrin A Action

E Billard, D Chatenet - ACS Medicinal Chemistry Letters, 2020 - ACS Publications
In the past few years, we have identified two allosteric modulators of the urotensinergic
system with probe-dependent action, termed Urocontrin (UC) and Urocontrin A (UCA). Such …

Membrane-tethered peptides derived from intracellular loops 2 and 3 of the urotensin II receptor act as allosteric biased ligands

H Nassour, TA Hoang, RD Martin, JCC Dallagnol… - bioRxiv, 2020 - biorxiv.org
Over the last decade, the urotensinergic system has garnered significant attention as a
promising new target for the treatment of various cardiovascular diseases and also cancer …